CN113943294A - 一种作为btk抑制剂的化合物及其制备方法与用途 - Google Patents

一种作为btk抑制剂的化合物及其制备方法与用途 Download PDF

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Publication number
CN113943294A
CN113943294A CN202011337022.9A CN202011337022A CN113943294A CN 113943294 A CN113943294 A CN 113943294A CN 202011337022 A CN202011337022 A CN 202011337022A CN 113943294 A CN113943294 A CN 113943294A
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China
Prior art keywords
substituted
cancer
unsubstituted
reaction
compound
Prior art date
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Pending
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CN202011337022.9A
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English (en)
Chinese (zh)
Inventor
岳春超
刘冠锋
李筛
李静
陈岗
原晨光
李英富
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shenzhen Haibowei Pharmaceutical Co ltd
Chengdu Haibowei Pharmaceutical Co ltd
Original Assignee
Shenzhen Haibowei Pharmaceutical Co ltd
Chengdu Haibowei Pharmaceutical Co ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shenzhen Haibowei Pharmaceutical Co ltd, Chengdu Haibowei Pharmaceutical Co ltd filed Critical Shenzhen Haibowei Pharmaceutical Co ltd
Priority to US18/014,157 priority Critical patent/US20230364079A1/en
Priority to CA3185574A priority patent/CA3185574A1/en
Priority to EP21842329.1A priority patent/EP4186906A1/en
Priority to EP21842091.7A priority patent/EP4186905A1/en
Priority to PCT/CN2021/105961 priority patent/WO2022012510A1/zh
Priority to CN202180037168.8A priority patent/CN116113633A/zh
Priority to CN202180037167.3A priority patent/CN115989231A/zh
Priority to PCT/CN2021/105960 priority patent/WO2022012509A1/zh
Priority to JP2023502793A priority patent/JP2023533350A/ja
Priority to KR1020237004806A priority patent/KR20230038530A/ko
Priority to US18/014,156 priority patent/US20230257383A1/en
Priority to JP2023502792A priority patent/JP2023533349A/ja
Priority to AU2021307502A priority patent/AU2021307502A1/en
Priority to TW110131533A priority patent/TWI826819B/zh
Priority to TW110131692A priority patent/TWI789886B/zh
Publication of CN113943294A publication Critical patent/CN113943294A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
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  • Oncology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202011337022.9A 2020-07-15 2020-11-25 一种作为btk抑制剂的化合物及其制备方法与用途 Pending CN113943294A (zh)

Priority Applications (15)

Application Number Priority Date Filing Date Title
US18/014,157 US20230364079A1 (en) 2020-07-15 2021-07-13 Compound as brain-permeable btk or her2 inhibitor, preparation method therefor, and use thereof
CA3185574A CA3185574A1 (en) 2020-07-15 2021-07-13 Compound serving as btk inhibitor, preparation method therefor, and use thereof
EP21842329.1A EP4186906A1 (en) 2020-07-15 2021-07-13 Compound as brain-permeable btk or her2 inhibitor, preparation method therefor, and use thereof
EP21842091.7A EP4186905A1 (en) 2020-07-15 2021-07-13 Compound serving as btk inhibitor, preparation method therefor, and use thereof
PCT/CN2021/105961 WO2022012510A1 (zh) 2020-07-15 2021-07-13 一种作为btk抑制剂的化合物及其制备方法与用途
CN202180037168.8A CN116113633A (zh) 2020-07-15 2021-07-13 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途
CN202180037167.3A CN115989231A (zh) 2020-07-15 2021-07-13 一种作为btk抑制剂的化合物及其制备方法与用途
PCT/CN2021/105960 WO2022012509A1 (zh) 2020-07-15 2021-07-13 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途
JP2023502793A JP2023533350A (ja) 2020-07-15 2021-07-13 脳透過性btk又はher2阻害剤としての化合物およびその製造方法と応用
KR1020237004806A KR20230038530A (ko) 2020-07-15 2021-07-13 Btk 억제제로서 역할을 하는 화합물, 이의 제조방법 및 이의 용도
US18/014,156 US20230257383A1 (en) 2020-07-15 2021-07-13 Compound serving as btk inhibitor, preparation method therefor, and use thereof
JP2023502792A JP2023533349A (ja) 2020-07-15 2021-07-13 Btk阻害剤としての化合物およびその製造方法と応用
AU2021307502A AU2021307502A1 (en) 2020-07-15 2021-07-13 Compound serving as BTK inhibitor, preparation method therefor, and use thereof
TW110131533A TWI826819B (zh) 2020-07-15 2021-08-25 一種作為btk抑制劑的化合物及其製備方法與用途
TW110131692A TWI789886B (zh) 2020-07-15 2021-08-26 一種作為可透腦的btk或her2抑制劑的化合物及其製備方法與用途

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2020106797766 2020-07-15
CN202010679776 2020-07-15

Publications (1)

Publication Number Publication Date
CN113943294A true CN113943294A (zh) 2022-01-18

Family

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Family Applications (3)

Application Number Title Priority Date Filing Date
CN202011337022.9A Pending CN113943294A (zh) 2020-07-15 2020-11-25 一种作为btk抑制剂的化合物及其制备方法与用途
CN202180037168.8A Pending CN116113633A (zh) 2020-07-15 2021-07-13 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途
CN202180037167.3A Pending CN115989231A (zh) 2020-07-15 2021-07-13 一种作为btk抑制剂的化合物及其制备方法与用途

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN202180037168.8A Pending CN116113633A (zh) 2020-07-15 2021-07-13 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途
CN202180037167.3A Pending CN115989231A (zh) 2020-07-15 2021-07-13 一种作为btk抑制剂的化合物及其制备方法与用途

Country Status (9)

Country Link
US (2) US20230257383A1 (ko)
EP (2) EP4186905A1 (ko)
JP (2) JP2023533350A (ko)
KR (1) KR20230038530A (ko)
CN (3) CN113943294A (ko)
AU (1) AU2021307502A1 (ko)
CA (1) CA3185574A1 (ko)
TW (2) TWI826819B (ko)
WO (2) WO2022012509A1 (ko)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115443277A (zh) * 2020-03-12 2022-12-06 重庆复尚源创医药技术有限公司 作为激酶抑制剂的化合物

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023510212A (ja) * 2020-01-02 2023-03-13 ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド Btk阻害薬

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GB9414974D0 (en) * 1994-07-26 1994-09-14 Bnfl Fluorchem Ltd Selectively fluorinated organic compounds
JP2011520970A (ja) * 2008-05-19 2011-07-21 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換されたイミダゾピラジン類およびイミダゾトリアジン類
US7718662B1 (en) * 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
CA2918242C (en) * 2013-07-31 2022-06-21 Merck Patent Gmbh Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof
CN105017256A (zh) * 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
WO2016106652A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors
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CN106243133A (zh) * 2016-07-28 2016-12-21 天津师范大学 具有氢气吸附性质的蒽环双三唑锌配合物单晶与应用
CN111454268B (zh) * 2019-01-18 2023-09-08 明慧医药(上海)有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
CN113365631A (zh) * 2019-01-18 2021-09-07 杭州邦顺制药有限公司 布鲁顿酪氨酸激酶抑制剂
JP2023510212A (ja) * 2020-01-02 2023-03-13 ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド Btk阻害薬

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115443277A (zh) * 2020-03-12 2022-12-06 重庆复尚源创医药技术有限公司 作为激酶抑制剂的化合物

Also Published As

Publication number Publication date
CA3185574A1 (en) 2022-01-20
TWI789886B (zh) 2023-01-11
JP2023533349A (ja) 2023-08-02
WO2022012509A1 (zh) 2022-01-20
KR20230038530A (ko) 2023-03-20
EP4186906A1 (en) 2023-05-31
CN115989231A (zh) 2023-04-18
US20230257383A1 (en) 2023-08-17
WO2022012510A1 (zh) 2022-01-20
JP2023533350A (ja) 2023-08-02
TW202220995A (zh) 2022-06-01
CN116113633A (zh) 2023-05-12
EP4186905A1 (en) 2023-05-31
AU2021307502A1 (en) 2023-02-09
TWI826819B (zh) 2023-12-21
TW202220996A (zh) 2022-06-01
US20230364079A1 (en) 2023-11-16

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